A cell-permeable inhibitor of Epac1 and Epac2 (IC50 = 5.9 µM for Epac2); inhibits Epac1-mediated Rap1-GDP exchange activity at 25 µM

HJC0197 – 5 mg

Brand:
Cayman
CAS:
1383539-73-8
Storage:
-20
UN-No:
Non-Hazardous - /

Exchange protein activated by cAMP (Epac) proteins mediate cAMP signaling independent of protein kinase A (PKA). HJC0197 is a cell-permeable inhibitor of Epac1 and Epac2 (IC50 = 5.9 µM for Epac2).{30769} It inhibits Epac1-mediated Rap1-GDP exchange activity at 25 µM, but has no effect on cAMP-induced type I and II PKA activity at this concentration.{30769} Pretreatment of HEK293 cells expressing either Epac1 or Epac2 with 10 µM HJC0197 completely blocks Epac-mediated phosphorylation of Akt.{30769} HJC0197 has been used to study the role of Epac signaling in chondrogenesis in chicken micromass cultures.{30770}  

 

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Description

A cell-permeable inhibitor of Epac1 and Epac2 (IC50 = 5.9 µM for Epac2); inhibits Epac1-mediated Rap1-GDP exchange activity at 25 µM, but has no effect on PKA activity; blocks Epac-mediated phosphorylation of Akt in HEK293 cells expressing either Epac1 or Epac2

Formal name: 4-​cyclopentyl-​2-​[[(2,​5-​dimethylphenyl)​methyl]​thio]​-​1,​6-​dihydro-​6-​oxo-5-pyrimidinecarbonitri​le

Synonyms: 

Molecular weight: 339.5

CAS: 1383539-73-8

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors||Research Area|Cell Biology|Cell Signaling|cAMP Signaling

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